产品
编 号：F760534
分子式：C19H11ClF3N5OS
分子量：449.84
分子式：C19H11ClF3N5OS
分子量：449.84
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 825658-63-7
产品详情
生物活性：
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD).
体内研究：
RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist).RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes.Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes.specieshalf-life (min) clearance, CLINT (mL/min/mg)
Human83.914.9
Rat9.11274
Mouse65.863.5
体外研究：
RTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (Ki=1 μM) and a very weak affinity for human sigma 2 (Ki=8.4 μM).
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD).
体内研究：
RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist).RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes.Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes.specieshalf-life (min) clearance, CLINT (mL/min/mg)
Human83.914.9
Rat9.11274
Mouse65.863.5
体外研究：
RTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (Ki=1 μM) and a very weak affinity for human sigma 2 (Ki=8.4 μM).
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